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1.
Geriatr Nurs ; 50: 165-173, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36780714

RESUMO

Postoperative pulmonary complications (PPCs) are a major catastrophic consequence of upper abdominal surgery, resulting in morbidity and mortality. Therefore, the study aims to assess the effect of lung expansion modalities (LEMs) on older adults' pulmonary function and the incidence of pulmonary complications. The study randomly allocated 80 older adults (40 cases and 40 controls). Pulmonary function testing revealed a significant improvement in the study group's forced expiratory volume in one second, sixth second, and oxygen saturation on the fifth postoperative day (POD) compared to the first day [55.23%, 38.41%, and 2.87%; P0.001]. The reported PPCs incidence of the intervention group was less than the control group (15% and 30% on the third POD; 15% and 37.5% on the fifth POD). In conclusion, LEMs provide practical enhancement for the postoperative care of older adults by reducing PPCs by restoring measured pulmonary volumes.


Assuntos
Pulmão , Complicações Pós-Operatórias , Humanos , Idoso , Complicações Pós-Operatórias/prevenção & controle , Complicações Pós-Operatórias/epidemiologia
2.
J Enzyme Inhib Med Chem ; 35(1): 847-863, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32216479

RESUMO

Oxidative stress is one of the main causes of significant severe diseases. The discovery of new potent antioxidants with high efficiency and low toxicity is a great demand in the field of medicinal chemistry. Herein, we report the design, synthesis molecular modelling and biological evaluation of novel hybrids containing pyrazole, naphthalene and pyrazoline/isoxazoline moiety. Chalcones 2a-e were synthesized efficiently and were used as starting materials for synthesis of a variety of heterocycles. A novel series of pyrazoline 3a-e, phenylpyrazoline 4a-e, isoxazoline 5a-e and pyrazoline carbothioamide derivatives 6a-e were synthesized and screened for in vitro antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and superoxide radical scavenging assay as well as 15-lipoxygenase (15-LOX) inhibition activity. Compounds 3a, 4e, 5b, 5c, 6a, 6c, and 6e showed excellent radical scavenging activity in all three methods in comparison with ascorbic acid and 15-LOX inhibition potency using quercetin as standard then were subjected to in vivo study. Catalase (CAT) activity, glutathione (GSH) and malondialdehyde (MDA) levels were assayed in liver of treated rats. Compounds 5b, 5c, and 6e showed significant in vivo antioxidant potentials compared to control group at dose of 100 mg/kg B.W. Molecular docking of compound 6a endorsed its proper binding at the active site pocket of the human 15-LOX which explains its potent antioxidant activity in comparison with standard ascorbic acid.


Assuntos
Antioxidantes/farmacologia , Araquidonato 15-Lipoxigenase/metabolismo , Desenho de Fármacos , Inibidores de Lipoxigenase/farmacologia , Pirazóis/farmacologia , Animais , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Relação Dose-Resposta a Droga , Humanos , Inibidores de Lipoxigenase/síntese química , Inibidores de Lipoxigenase/química , Masculino , Modelos Moleculares , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Picratos/antagonistas & inibidores , Pirazóis/síntese química , Pirazóis/química , Ratos , Ratos Wistar , Relação Estrutura-Atividade , Superóxidos/antagonistas & inibidores
3.
J Enzyme Inhib Med Chem ; 34(1): 1110-1120, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31117890

RESUMO

New anticancer agents are highly needed to overcome cancer cell resistance. A novel series of pyrimidine pyrazoline-anthracene derivatives (PPADs) (4a-t) were designed and synthesised. The anti-liver cancer activity of all compounds was screened in vitro against two hepatocellular carcinoma (HCC) cell lines (HepG2 and Huh-7) as well as normal fibroblast cells by resazurin assay. The designed compounds 4a-t showed a broad-spectrum anticancer activity against the two cell lines and their activity was more prominent on cancer compared to normal cells. Compound 4e showed high potency against HepG2 and Huh-7 cell lines ((IC50=5.34 and 6.13 µg/mL, respectively) comparable to that of doxorubicin (DOX) activities. A structure activity relationship (SAR) has been investigated and compounds 4e, 4i, 4m, and 4q were the most promising anticancer agents against tested cell lines. These compounds induced apoptosis in HepG2 and Huh-7 cells through significant activation of caspase 3/7 at all tested concentrations. In conclusion, 4e could be a potent anticancer drug.


Assuntos
Antineoplásicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Desenho de Fármacos , Neoplasias Hepáticas/tratamento farmacológico , Pirimidinas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Caspase 3/metabolismo , Caspase 7/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Modelos Moleculares , Estrutura Molecular , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade
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